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In vitro: BAR 501 is a selective GPBAR1 agonist devoid of FXR agonistic activity. It effectively transactivates GPBAR1 in HEK293 cells overexpressing a CRE along with GPBAR1, with an EC50 of 1 μM. Exposure of GLUTAg cells to BAR501 (10 μM) increases the expression of GLP-1 mRNA by 2.5 folds.
In vivo: Pretreating rats for 6 days with BAR501, 15 mg/kg, reduces basal portal pressure and blunts the vasoconstriction activity of norepinephrine. Pretreatment with BAR501 attenuates the hepatic vasomotor activity induced by shear stress and methoxamine. Administration of BAR501 exerts a direct vasodilatory activity in the CCl4 model. Treating mice with BAR501 at the dose of 15 mg/Kg reduces portal pressure and AST plasma levels. BAR501 attenuates endothelial dysfunction by regulating CSE expression/activity.
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| Cell lines | |
| Preparation method | |
| Concentrations | |
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| Animal Experiment | |
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| Animal models | Mice bearing GM-CSF-secreting B16 tumors |
| Formulation | 5% DMA, 47.5% propylene glycol |
| Dosages | 75 mg/kg b.i.d |
| Administration | s.c. |
| Molecular Weight | 406.64 |
| Formula | C26H46O3 |
| CAS Number | 1632118-69-4 |
| Solubility (25°C) | 10mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CGRP Receptor Products |
|---|
| MK-3207 hydrochloride
MK-3207 hydrochloride is a potent CGRP receptor antagonist with IC50 of 0.12 nM. |
| Rimegepant
Rimegepant, also known as BMS-927711, is a potent, selective, competitive, and orally active calcitonin gene-related peptide (CGRP) antagonist with a Ki value of 0.027 nM. |
| BAR 501 impurity |
| MK-0974
MK-0974 (Telcagepant) is a highly potent, selective and orally bioavailable CGRP receptor antagonist with Ki values of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors respectively. |
| Olcegepant (BIBN-4096)
Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide (CGRP) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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